ECSP078004A - PREPARACIÓN y USO DE COMPUESTOS COMO INHIBIDORES DE PROTEASAS - Google Patents

PREPARACIÓN y USO DE COMPUESTOS COMO INHIBIDORES DE PROTEASAS

Info

Publication number
ECSP078004A
ECSP078004A EC2007008004A ECSP078004A ECSP078004A EC SP078004 A ECSP078004 A EC SP078004A EC 2007008004 A EC2007008004 A EC 2007008004A EC SP078004 A ECSP078004 A EC SP078004A EC SP078004 A ECSP078004 A EC SP078004A
Authority
EC
Ecuador
Prior art keywords
compounds
ring
bond
preparation
heterocyclyl
Prior art date
Application number
EC2007008004A
Other languages
English (en)
Inventor
Zhaoning Zhu
Tao Guo
Andrew Stamford
Brian Mckittrick
William Greenlee
Robert Mazzola
Thuy X H Le
Ying Huang
Gang Qian
Yuefei Shao
Guoqing Li
Original Assignee
Schering Corp
Pharmacopeia Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corp, Pharmacopeia Inc filed Critical Schering Corp
Publication of ECSP078004A publication Critical patent/ECSP078004A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • AIDS & HIV (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Se revelan los compuestos de la fórmula I Io un estereoisómero, tautómero o sal o solvato del mismo aceptable para uso farmacéutico, donde Q es un enlace o -N(R5)-;T es un enlace , -O-, -C(O)-, S, -N(R5)- o -C(R6'R7');U es un enlace o -C(R6)(R7)-; Y es C o N;Z es C o N;el anillo A, que incluye las variables Y y Z, es un anillo cicloalquilo, cicloalquenilo, heterociclilo, heterociclenilarilo y heteroarilo de tres a nueve miembros que tiene 0 a 4, con preferencia 0 a 2, heteroátomos seleccionados independientemente del grupo que consiste en O, S, N y -N(R)-, donde el anillo A está no sustituido o sustituido con 1 a 5 residuos R1 seleccionados independientemente y/u oxo cuando el anillo A es cicloalquilo, cicloalquenilo, heterociclilo o heterociclenilo; y R, R1, R2, R3, R4, R5, R6, R6, R7 y R7' son tal como se definen en la memoria descriptiva; composiciones farmacéuticas que comprenden los compuestos de la fórmula I y el método para inhibir aspartil proteasas y, en particular, los métodos para tratar enfermedades cardiovasculares, enfermedades cognitivas y neurodegenerativas .
EC2007008004A 2005-06-14 2007-12-12 PREPARACIÓN y USO DE COMPUESTOS COMO INHIBIDORES DE PROTEASAS ECSP078004A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US69054105P 2005-06-14 2005-06-14

Publications (1)

Publication Number Publication Date
ECSP078004A true ECSP078004A (es) 2008-01-23

Family

ID=37467438

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2007008004A ECSP078004A (es) 2005-06-14 2007-12-12 PREPARACIÓN y USO DE COMPUESTOS COMO INHIBIDORES DE PROTEASAS

Country Status (19)

Country Link
US (2) US8722708B2 (es)
EP (2) EP2345411B1 (es)
JP (2) JP4896972B2 (es)
KR (1) KR20080028881A (es)
CN (1) CN101394852A (es)
AR (1) AR056865A1 (es)
AU (1) AU2006259573A1 (es)
BR (1) BRPI0612545A2 (es)
CA (1) CA2610828A1 (es)
EC (1) ECSP078004A (es)
ES (1) ES2436795T3 (es)
IL (1) IL187455A0 (es)
MX (1) MX2007016183A (es)
NO (1) NO20080186L (es)
PE (1) PE20070321A1 (es)
RU (1) RU2008100164A (es)
TW (1) TW200716643A (es)
WO (1) WO2006138265A2 (es)
ZA (1) ZA200710385B (es)

Families Citing this family (71)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7700603B2 (en) 2003-12-15 2010-04-20 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7592348B2 (en) 2003-12-15 2009-09-22 Schering Corporation Heterocyclic aspartyl protease inhibitors
JP2008543840A (ja) 2005-06-14 2008-12-04 シェーリング コーポレイション アスパルチルプロテアーゼインヒビター
EP1896478B1 (en) 2005-06-14 2014-05-21 Merck Sharp & Dohme Corp. Aspartyl protease inhibitors
KR101052122B1 (ko) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 아미노디히드로티아진 유도체
EP2032542A2 (en) 2006-06-12 2009-03-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815349A (en) * 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
CN101631779A (zh) * 2006-12-12 2010-01-20 先灵公司 含有三环***的天冬氨酰蛋白酶抑制剂
US8093254B2 (en) 2006-12-12 2012-01-10 Schering Corporation Aspartyl protease inhibitors
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
TW200902499A (en) * 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
WO2009005471A1 (en) * 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005470A1 (en) * 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
CA2698341A1 (en) 2007-09-06 2009-03-12 Schering Corporation Gamma secretase modulators
CA2704698A1 (en) 2007-11-05 2009-05-14 Schering Corporation Gamma secretase modulators
WO2009076352A1 (en) 2007-12-11 2009-06-18 Schering Corporation Gamma secretase modulators
EA019156B1 (ru) 2008-02-01 2014-01-30 Такеда Фармасьютикал Компани Лимитед Производные оксима в качестве ингибиторов hsp90
CN102119161B (zh) 2008-06-13 2015-07-08 盐野义制药株式会社 具有β分泌酶抑制作用的含硫杂环衍生物
TWI385175B (zh) 2008-09-11 2013-02-11 Amgen Inc 作為β-分泌酶調節劑之螺旋-三環化合物及其使用方法
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
CA2742486A1 (en) 2008-11-13 2010-05-20 Schering Corporation Gamma secretase modulators
TW201020244A (en) * 2008-11-14 2010-06-01 Astrazeneca Ab New compounds
WO2010056195A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
WO2010056194A1 (en) * 2008-11-14 2010-05-20 Astrazeneca Ab 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use
CA2747750A1 (en) 2008-12-22 2010-07-01 Theodros Asberom Gamma secretase modulators
WO2010075203A1 (en) 2008-12-22 2010-07-01 Schering Corporation Gamma secretase modulators
EP2443119A1 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
US20120238546A1 (en) 2009-06-16 2012-09-20 Zhaoning Zhu Gamma secretase modulators
EP2443118A1 (en) 2009-06-16 2012-04-25 Schering Corporation Gamma secretase modulators
EP2281824A1 (en) 2009-08-07 2011-02-09 Noscira, S.A. Furan-imidazolone derivatives, for the treatment of cognitive, neurodegenerative or neuronal diseases or disorders
WO2011044187A1 (en) 2009-10-08 2011-04-14 Schering Corporation Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
WO2011044185A2 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
UA108363C2 (uk) 2009-10-08 2015-04-27 Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування
WO2011044184A1 (en) 2009-10-08 2011-04-14 Schering Corporation Pentafluorosulfur imino heterocyclic compounds as bace-1 inhibitors, compositions, and their use
MX2012006491A (es) 2009-12-11 2012-07-03 Shionogi & Co Derivados de oxazina.
EP2547686B1 (en) 2010-03-15 2014-01-22 Amgen Inc. Amino-dihydrooxazine and amino-dihydrothiazine spiro compounds as beta-secretase modulators and their medical use
MX2012010658A (es) 2010-03-15 2012-12-05 Amgen Inc Compuestos de anillo espiro tetraciclico como moduladores de beta-secretasa.
US20130109683A1 (en) 2010-06-09 2013-05-02 Janssen Pharmaceutica Nv 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace)
EP2601197B1 (en) 2010-08-05 2014-06-25 Amgen Inc. Amino-iso-indole, amino-aza-iso-indole, amino-dihydroisoquinoline and amino-benzoxazine compounds as beta-secretase modulators and methods of use
EP2619207B1 (en) * 2010-09-22 2014-11-12 Janssen Pharmaceutica, N.V. 4,7-Dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta secretase (BACE)
CN103261199A (zh) 2010-10-29 2013-08-21 盐野义制药株式会社 萘啶衍生物
WO2012057247A1 (ja) 2010-10-29 2012-05-03 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
WO2012069428A1 (en) 2010-11-22 2012-05-31 Noscira, S.A. Bipyridine sulfonamide derivatives for the treatment of neurodegenerative diseases or conditions
WO2012071279A1 (en) 2010-11-23 2012-05-31 Amgen Inc. Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
BR112013015430A2 (pt) 2010-12-22 2016-09-20 Janssen Pharmaceutica Nv derivados de 5,6-diidro-imidazo[1,2-a]pirazin-8-ilamina úteis como inibidores de beta-secretase (bace)
EP2673279A1 (en) 2011-02-07 2013-12-18 Amgen Inc. 5-amino-oxazepine and 5-amino-thiazepane compounds as beta-secretase antagonists and methods of use
EP2675810A1 (en) 2011-02-15 2013-12-25 Amgen Inc. Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
ES2558779T3 (es) 2011-03-01 2016-02-08 Janssen Pharmaceutica, N.V. Derivados de 6,7-dihidro-pirazolo[1,5-a]piracin-4-ilamina útiles como inhibidores de ß-secretasa (BACE)
MY163346A (en) 2011-03-09 2017-09-15 Janssen Pharmaceutica Nv 3,4-dihydro-pyrrolo[1,2-a]pyrazin-1-ylamine derivatives useful as inhibitors of beta-secretase (base)
US9221839B2 (en) 2011-04-07 2015-12-29 Merck Sharp & Dohme Corp. C5-C6 oxacyclic-fused thiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
WO2012138590A1 (en) 2011-04-07 2012-10-11 Merck Sharp & Dohme Corp. Pyrrolidine-fused thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
JPWO2012147763A1 (ja) 2011-04-26 2014-07-28 塩野義製薬株式会社 オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤
CN103874496A (zh) 2011-08-22 2014-06-18 默沙东公司 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途
US9296759B2 (en) 2011-09-21 2016-03-29 Amgen Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
AU2013235422B2 (en) 2012-03-19 2016-12-15 Buck Institute For Research On Aging APP specific BACE inhibitors (ASBIs) and uses thereof
EP2908825B1 (en) 2012-10-17 2018-04-18 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use
US9416129B2 (en) 2012-10-17 2016-08-16 Merck Sharp & Dohme Corp. Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
US9540359B2 (en) 2012-10-24 2017-01-10 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having BACE1 inhibitory activity
US9725469B2 (en) 2012-11-15 2017-08-08 Amgen, Inc. Amino-oxazine and amino-dihydrothiazine compounds as beta-secretase modulators and methods of use
JP6471100B2 (ja) 2013-02-12 2019-02-13 バック・インスティテュート・フォー・リサーチ・オン・エイジング Ｂａｃｅ仲介性ａｐｐプロセシングを調節するヒダントイン
US9663475B2 (en) 2013-02-25 2017-05-30 Merck Patent Gmbh 2 amino-3,4-dihydrcquinazoline derivatives and the use thereof as cathepsin D inhibitors
ES2627633T3 (es) 2013-06-12 2017-07-28 Janssen Pharmaceutica N.V. Derivados de 4-amino-6-fenil-5,6-dihidroimidazo[1,5-a]piracin-3(2H)-ona como inhibidores de beta-secretasa (BACE)
JP6325092B2 (ja) 2013-06-12 2018-05-16 ヤンセン ファーマシューティカ エヌ．ベー． βーセクレターゼ（ＢＡＣＥ）の阻害剤としての４−アミノ−６−フェニル−５，６−ジヒドロイミダゾ［１，５−Ａ］ピラジン誘導体
WO2014198854A1 (en) 2013-06-12 2014-12-18 Janssen Pharmaceutica Nv 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)
KR20170095881A (ko) 2014-12-18 2017-08-23 얀센 파마슈티카 엔.브이. 베타―세크레타제의 ２,３,４,５―테트라히드로피리딘―６―아민 및 ３,４―디히드로―２ｈ―피롤―５―아민 화합물 억제제
RU2642246C2 (ru) * 2014-12-30 2018-01-24 Федеральное государственное бюджетное научное учреждение "Институт экспериментальной медицины" (ФГБНУ "ИЭМ") Применение пробиотического штамма микроорганизма enterococcus faecium l-3 для лечения нейродегенеративных заболеваний
US20200069691A1 (en) * 2016-12-22 2020-03-05 Merck Sharp & Dohme Corp. Heterocyclic compounds as hiv protease inhibitors
JOP20180094A1 (ar) 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
CN110563631B (zh) * 2018-06-05 2023-05-23 爱斯特（成都）生物制药股份有限公司 一种抑制ido的化合物及其应用

Family Cites Families (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1077204A (en) 1912-11-20 1913-10-28 John Bonner Semple Tracer for projectiles.
US3632814A (en) * 1968-11-25 1972-01-04 Velsicol Chemical Corp Phosphoramidate esters
JPS5013951B1 (es) * 1969-05-23 1975-05-23
DE2430354A1 (de) * 1974-06-25 1976-01-15 Basf Ag Neue substituierte 1-amino-isoindole, verfahren zu deren herstellung sowie diese enthaltende pharmazeutische zubereitungen
DE2757982C2 (de) * 1977-12-24 1980-02-21 Basf Ag, 6700 Ludwigshafen Verbindungen der Isoindolinreihe und Verfahren zur Herstellung von in den anwendungstechnischen Eigenschaften verbesserten Pigmenten
DE3371618D1 (en) * 1982-02-27 1987-06-25 Asahi Chemical Ind Coloring method and color-forming material
IL92011A0 (en) * 1988-10-19 1990-07-12 Abbott Lab Heterocyclic peptide renin inhibitors
WO1993004047A1 (en) 1991-08-16 1993-03-04 Merck & Co., Inc. Quinazoline derivatives as inhibitors of hiv reverse transcriptase
DE4419849A1 (de) * 1994-06-07 1995-12-14 Hoechst Ag Isoindolinpigmente
US5629322A (en) * 1994-11-15 1997-05-13 Merck & Co., Inc. Cyclic amidine analogs as inhibitors of nitric oxide synthase
JP3666922B2 (ja) * 1995-02-21 2005-06-29 山本化成株式会社 カルボン酸塩、その製造方法および該塩化合物を用いる感熱記録材料
IL117149A0 (en) 1995-02-23 1996-06-18 Schering Corp Muscarinic antagonists
US5889006A (en) 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
DE19516804A1 (de) * 1995-05-08 1996-11-14 Hoechst Ag Isoindolinpigmente auf Basis von Aminochinoxalindionen
US5935958A (en) 1996-07-01 1999-08-10 Schering Corporation Muscarinic antagonists
US5952349A (en) 1996-07-10 1999-09-14 Schering Corporation Muscarinic antagonists for treating memory loss
US5977138A (en) 1996-08-15 1999-11-02 Schering Corporation Ether muscarinic antagonists
AU9298098A (en) * 1997-09-03 1999-03-22 Guilford Pharmaceuticals Inc. Amino-substituted compounds, methods, and compositions for inhibiting parp activity
WO1999033795A1 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
US6066636A (en) 1998-06-30 2000-05-23 Schering Corporation Muscarinic antagonists
US6420364B1 (en) * 1999-09-13 2002-07-16 Boehringer Ingelheim Pharmaceuticals, Inc. Compound useful as reversible inhibitors of cysteine proteases
ES2199856T3 (es) * 1999-09-13 2004-03-01 Boehringer Ingelheim Pharmaceuticals, Inc. Nuevos compuestos heterociclicos, utiles como inhibidores reversibles de cisteina proteasas.
US6294554B1 (en) 1999-09-22 2001-09-25 Schering Corporation Muscarinic antagonists
PE20020276A1 (es) * 2000-06-30 2002-04-06 Elan Pharm Inc COMPUESTOS DE AMINA SUSTITUIDA COMO INHIBIDORES DE ß-SECRETASA PARA EL TRATAMIENTO DE ALZHEIMER
EP1343760B1 (en) 2000-12-22 2009-08-12 Schering Corporation Muscarinic antagonists
AU2002306734A1 (en) 2001-03-15 2002-10-03 The Johns Hopkins University Inhibitors of plasmepsins
WO2003014075A2 (en) * 2001-08-03 2003-02-20 Schering Corporation Novel gamma secretase inhibitors
CN1301972C (zh) 2001-10-10 2007-02-28 先灵公司 作为毒覃碱拮抗剂的哌啶化合物
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
AU2004299040A1 (en) * 2003-12-15 2005-06-30 Pharmacopeia, Inc. Heterocyclic aspartyl protease inhibitors
ATE444962T1 (de) * 2004-06-16 2009-10-15 Wyeth Corp Amino-5,5-diphenylimidazolon-derivate zur beta- sekretase-hemmung
RU2006144075A (ru) * 2004-06-16 2008-07-27 Вайет (Us) ДИФЕНИЛИМИДАЗОПИРИМИДИН И -ИМИДАЗОЛАМИНЫ КАК ИНГИБИТОРЫ β-СЕКРЕТАЗЫ
WO2006017844A1 (en) 2004-08-06 2006-02-16 Janssen Pharmaceutica, N.V. NOVEL 2-AMINO-QUINAZOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
EP1789398B1 (en) 2004-08-06 2010-09-29 Janssen Pharmaceutica NV 2-amino-quinazoline derivatives useful as inhibitors of b-secretase (bace)
EP1804794B1 (en) 2004-10-13 2013-07-31 Merck Sharp & Dohme Corp. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer s disease
WO2006044492A2 (en) 2004-10-14 2006-04-27 Ingenious Targeting Laboratory, Inc. Methods for generating rat embryo-derived cell lines and genetic modification of rat genome
WO2006041404A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Substituted amino-compounds and uses thereof
EP1802588A4 (en) * 2004-10-15 2010-02-17 Astrazeneca Ab SUBSTITUTED AMINOPYRIMIDONE AND APPLICATIONS THEREOF
CA2593515A1 (en) 2005-01-14 2006-07-20 Wyeth Amino-imidazolones for the inhibition of beta-secretase
CN101198597B (zh) 2005-06-14 2011-11-16 先灵公司 作为天冬氨酰基蛋白酶抑制剂的化合物的制备和用途
PE20070078A1 (es) * 2005-06-14 2007-03-08 Schering Corp Compuestos heterociclicos macrociclicos como inhibidores de aspartil proteasa
EP1896478B1 (en) 2005-06-14 2014-05-21 Merck Sharp & Dohme Corp. Aspartyl protease inhibitors
MX2008000212A (es) * 2005-06-30 2008-03-24 Wyeth Corp Compuestos amino-5-(6 miembros)heteroarilimidazolona y el uso de estos para la modulacion de la (-secretasa.
TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
TW200730523A (en) * 2005-07-29 2007-08-16 Wyeth Corp Cycloalkyl amino-hydantoin compounds and use thereof for β-secretase modulation
CN101273018A (zh) * 2005-09-26 2008-09-24 惠氏公司 用于β分泌酶（BACE）抑制剂的氨基-5-[4-(二氟甲氧基)苯基]-5-苯基咪唑酮化合物
KR101052122B1 (ko) 2005-10-25 2011-07-26 시오노기세야쿠 가부시키가이샤 아미노디히드로티아진 유도체
EP1966198B1 (en) * 2005-10-25 2011-03-16 Janssen Pharmaceutica NV 2-amino-3,4-dihydro-pyrido[3,4-d]pyrimidine derivatives useful as inhibitors of beta-secretase (bace)
ES2349433T3 (es) 2005-10-27 2011-01-03 Schering Corporation Inhibidores heterocíclicos de aspartil proteasa.
CN101351460A (zh) * 2005-10-31 2009-01-21 先灵公司 天冬氨酰蛋白酶抑制剂
TW200804290A (en) 2005-11-15 2008-01-16 Astrazeneca Ab Compounds and uses thereof
AR058381A1 (es) * 2005-12-19 2008-01-30 Astrazeneca Ab Compuestos derivados de 2-aminopiridin-4-onas y una composicion farmaceutica
WO2007092854A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007092839A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
US7776882B2 (en) 2006-02-06 2010-08-17 Baxter Ellen W 2-amino-3,4-dihydro-quinoline derivatives useful as inhibitors of β-secretase (BACE)
WO2007100536A1 (en) * 2006-02-24 2007-09-07 Wyeth DIHYDROSPIRO[DIBENZO[A,D][7]ANNULENE-5,4'-IMIDAZOL] COMPOUNDS FOR THE INHIBITION OF β-SECRETASE
CN101460480A (zh) 2006-04-05 2009-06-17 阿斯利康(瑞典)有限公司 2-氨基嘧啶-4-酮类化合物及其用于治疗或预防Aβ相关病理的用途
EP2032542A2 (en) * 2006-06-12 2009-03-11 Schering Corporation Heterocyclic aspartyl protease inhibitors
TW200815449A (en) * 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds II
TW200808796A (en) 2006-06-14 2008-02-16 Astrazeneca Ab New compounds III
TW200815443A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds I
TW200815447A (en) 2006-06-14 2008-04-01 Astrazeneca Ab Novel compounds IV
US20080051420A1 (en) * 2006-06-14 2008-02-28 Astrazeneca Ab New Compounds 317
TW200815349A (en) * 2006-06-22 2008-04-01 Astrazeneca Ab New compounds
TW200817406A (en) 2006-08-17 2008-04-16 Wyeth Corp Imidazole amines as inhibitors of β-secretase
WO2008063114A1 (en) 2006-11-20 2008-05-29 Astrazeneca Ab Amino- imidazolones and their use as medicament for treating cognitive impairment alzheimer disease, neurodegeneration and dementia
US8093254B2 (en) 2006-12-12 2012-01-10 Schering Corporation Aspartyl protease inhibitors
CN101631779A (zh) 2006-12-12 2010-01-20 先灵公司 含有三环***的天冬氨酰蛋白酶抑制剂
TW200831484A (en) * 2006-12-20 2008-08-01 Astrazeneca Ab New compounds
KR20100017255A (ko) 2007-04-24 2010-02-16 시오노기 앤드 컴파니, 리미티드 환식기로 치환된 아미노다이하이드로싸이아진 유도체
JP5383483B2 (ja) 2007-04-24 2014-01-08 塩野義製薬株式会社 アルツハイマー症治療用医薬組成物
TW200902499A (en) 2007-05-15 2009-01-16 Astrazeneca Ab New compounds
UY31083A1 (es) * 2007-05-15 2009-01-05 Astrazeneca Ab Derivados de sulfoximinas para la inhibicion de b-secretasa
WO2009005470A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009005471A1 (en) 2007-07-05 2009-01-08 Astrazeneca Ab Aryl and heteroaryl substituted isoindole derivatives as bace inhibitors
WO2009007300A2 (en) 2007-07-06 2009-01-15 Boehringer Ingelheim International Gmbh Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture
US20100317850A1 (en) 2008-01-18 2010-12-16 Yuichi Suzuki Condensed aminodihydrothiazine derivative
US8426607B2 (en) 2008-01-22 2013-04-23 Boehringer Ingelheim International Gmbh Substituted amino-benzimidazoles, medicaments comprimising said compound, their use and their method of manufacture
MX2010008202A (es) 2008-01-28 2010-12-06 Janssen Pharmaceutica Nv Derivados de tio-2-aminoquinolina 6-sustituida utiles como inhibidores de beta-secretasa (bace).
CA2714008A1 (en) 2008-01-29 2009-08-06 Janssen Pharmaceutica N.V. 2-amino quinoline derivatives useful as inhibitors of .beta.-secretase (bace)
JP5258904B2 (ja) * 2008-02-18 2013-08-07 エフ．ホフマン−ラ ロシュ アーゲー ４，５−ジヒドロオキサゾール−２−イルアミン誘導体
EP2257167B1 (en) 2008-02-28 2015-07-22 Merck Sharp & Dohme Corp. 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
US8450331B2 (en) 2008-04-22 2013-05-28 Merck Sharp & Dohme Corp. Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
TWI431004B (zh) 2008-05-02 2014-03-21 Lilly Co Eli Ｂａｃｅ抑制劑
CN102119161B (zh) 2008-06-13 2015-07-08 盐野义制药株式会社 具有β分泌酶抑制作用的含硫杂环衍生物
ES2433223T3 (es) 2008-07-28 2013-12-10 Eisai R&D Management Co., Ltd. Derivados de espiroaminodihidrotiazina
WO2010013302A1 (ja) 2008-07-28 2010-02-04 エーザイ・アール・アンド・ディー・マネジメント株式会社 スピロアミノジヒドロチアジン誘導体
MX2011003189A (es) 2008-09-30 2011-04-27 Eisai R&D Man Co Ltd Nuevo derivado de aminodihidrotiazina fusionada.
JPWO2010047372A1 (ja) 2008-10-22 2012-03-22 塩野義製薬株式会社 Ｂａｃｅ１阻害活性を有する２−アミノピリミジン−４−オンおよび２−アミノピリジン誘導体
WO2010056195A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab New compounds 575
WO2010056194A1 (en) 2008-11-14 2010-05-20 Astrazeneca Ab 5h-pyrrolo [ 3, 4-b] pyridin derivatives and their use
JP2012509352A (ja) 2008-11-20 2012-04-19 パーデュー・リサーチ・ファウンデーション Ｂａｃｅ１のキナゾリン阻害剤および使用方法

Also Published As

Publication number Publication date
EP2345411B1 (en) 2013-10-02
EP1896032B1 (en) 2012-10-31
US20080176868A1 (en) 2008-07-24
ZA200710385B (en) 2008-11-26
RU2008100164A (ru) 2009-07-20
EP2345411A1 (en) 2011-07-20
US8722708B2 (en) 2014-05-13
BRPI0612545A2 (pt) 2010-11-23
MX2007016183A (es) 2008-03-10
PE20070321A1 (es) 2007-04-16
CA2610828A1 (en) 2006-12-28
AR056865A1 (es) 2007-10-31
NO20080186L (no) 2008-03-14
KR20080028881A (ko) 2008-04-02
JP2008546696A (ja) 2008-12-25
TW200716643A (en) 2007-05-01
US20140206715A1 (en) 2014-07-24
JP5454956B2 (ja) 2014-03-26
CN101394852A (zh) 2009-03-25
AU2006259573A1 (en) 2006-12-28
WO2006138265A3 (en) 2007-03-01
ES2436795T3 (es) 2014-01-07
IL187455A0 (en) 2008-02-09
JP4896972B2 (ja) 2012-03-14
JP2011251978A (ja) 2011-12-15
EP1896032A2 (en) 2008-03-12
US9382242B2 (en) 2016-07-05
WO2006138265A2 (en) 2006-12-28

Similar Documents

Publication Publication Date Title
ECSP078004A (es) PREPARACIÓN y USO DE COMPUESTOS COMO INHIBIDORES DE PROTEASAS
NO20061822L (no) Makrosykliske inhibitorer av hepatitt C-virus-NS3-serinprotease
ATE433984T1 (de) Verbindungen und verfahren zur behandlung von dyslipidämie
AR067156A1 (es) DERIVADOS DE TETRAHIDRO-2H-PIRIDO(4,3-B)INDOL-2-ILO, UN PROCESO PARA SU PREPARACION, UNA COMPOSICION FARMACEUTICA QUE LOS COMPRENDE Y SU USO EN LA FABRICACIoN DE UN MEDICAMENTO PARA EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR LA INHIBICION DE CATEPSINA K
NO20083598L (no) Karbosykliske og heterosykliske arylsulfoner som inhibitorer av gamma-sekretase
NO20063205L (no) Inhibitorer for hepatitt C-virus NS3/NS4A-serinprotease
UY27503A1 (es) Nuevos derivados de piperazina
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
ECSP099597A (es) Inhibidores heterocíclicos de la aspartil proteasa
MX2009006227A (es) Inhibidores de aspartil proteasa que contienen un sistema de anillo triciclico.
UY28578A1 (es) Derivados de amida
AR077935A1 (es) Derivados de 3-amino-5 fenil-5,6-dihidro-2h-(1,4)oxazina
UY29301A1 (es) Derivados amida
NO20064355L (no) Nye ketoamider med sykliske P4-er som inhibitorer for NS3-serinprotease fra hepatitt C-virus
WO2006138230A3 (en) The preparation and use of protease inhibitors
NO20056192L (no) Kapaseinhibitorer og anvendelse derav
ECSP066640A (es) Inhibidores heterocíclicos de aspartil proteasa
NO20050635L (no) Nye tricykliske spiropiperidiner eller spiropyrrolidiner
ATE435855T1 (de) Verbindungen mit agonistischer wirkung am beta2- adrenergen rezeptor und am muscarinischen rezeptor
AR058885A1 (es) Compuestos de piperidina 3,5-sustituidos
AR049433A1 (es) Derivados de naftalina
NO20060383L (no) Substituerte diketopiperaziner og deres anvendelse som oksytocinantagonister
PE20090548A1 (es) Compuestos aza-biciclohexano como inhibidores de trombina
AR053435A1 (es) Derivados de 5-amminoindol, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un madicamento para el tratamiento de enfermedades asociadas a la modulacion de receptores h3.
NO20073170L (no) Kaspaseinhibitorer og anvendelse derav